Discovery of betulinic acid as a selective inhibitor of human melanoma that functions by induction of apoptosis

@article{Pisha1995DiscoveryOB,
  title={Discovery of betulinic acid as a selective inhibitor of human melanoma that functions by induction of apoptosis},
  author={Emily Pisha and Hee-byung Chai and Ik-Soo Lee and Tangai E. Chagwedera and N. R. Farnsworth and Geoffrey A. Cordell and Chris Beecher and Harry H. S. Fong and A. Douglas Kinghorn and Daniel M. Brown and Mansukh C. Wani and Monroe E. Wall and Tina J Hieken and Tapas K. Das Gupta and John M. Pezzuto},
  journal={Nature Medicine},
  year={1995},
  volume={1},
  pages={1046-1051}
}
As a result of bioassay–guided fractionation, betulinic acid, a pentacyclic triterpene, was identified as a melanoma–specific cytotoxic agent. In follow–up studies conducted with athymic mice carrying human melanomas, tumour growth was completely inhibited without toxicity. As judged by a variety of cellular responses, antitumour activity was mediated by the induction of apoptosis. Betulinic acid is inexpensive and available in abundant supply from common natural sources, notably the bark of… 
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  • Biology, Medicine
    Molecular nutrition & food research
  • 2009
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In contrast to the potent cytotoxicity of BA against a variety of cancer types, nonmalignant cells and normal tissue remained relatively resistant to BA, indicating a therapeutic window.
Betulinic acid inhibits prostate cancer growth through inhibition of specificity protein transcription factors.
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Cytotoxic betulin-derived hydroxypropargylamines trigger apoptosis.
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